PROCEDUR MANUAL LABORATORY

NEUROBEHAVIOUR SYSTEM

SECTION: PHARMACOLOGY

NEUROBEHAVIOUR SYSTEM

LAB. ACTIVITY OF PHARMACOLOGY & THERAPY

PHARMACOLOGICAL PROPERTIES OF

AUTONOMIC DRUGS

LABORATORY ACTIVITY PHARMACOLOGY

FOR STUDENT

Module author : Siti Annisa Devi Trusda, dr., M.Kes

Resource Person : Yuke Andriane,dr.,M.Kes

Subject : Pharmacological Properties of Autonomic Drugs

Department : Pharmacology

A Sequent

I Introduction : 40 menit

II Pretest : 5 menit

III Laboratory activity : 125 menit

IV Post test : -

B Topic : Pharmacological Properties of Autonomic Drugs

Date: October 2019

1. Discussion about pharmacological properties of autonomic

drugs

2. Poster

3. Case Discussion

:

:

:

30 menit

50 menit

45 menit

C Venue

Biomedical Laboratory, Faculty of Medicine, Unisba, Jl. Tamansari No.22 Bandung 40116

D Equipment

1 Discussion about pharmacological properties of

autonomic drugs

1. Task

2. Text book

3. Modul

4. MIMS

2 Poster 1. Posters

3 Case Discussion 1. Cases

2. Text book

3. MIMS

E Pre-requisite/ Pretest and Task

Before laboratory activity students should have initial knowledge about:

Task To be collected to your tutor at the day of Lab. Activity 1. Explain the adrenergic and cholinergic transmission!

2. Explain the cellular effects and the distribution of each adrenoceptors!

3. Explain the pharmacological properties of adrenergic agonist and adrenergic antagonist!

4. Explain the cellular effects and the distribution of each cholinoceptor!

5. Explain the pharmacological properties of cholinergic drug!

Note:

If the pre-test score less than 50, the student will get additional assignments.

F Implementation

1. Students are divided into 17 groups

2. Each group is supervised by one tutor

Activity 1 : Discussion about pharmacological properties of autonomic drugs

The motor (efferent) portion of the nervous system can be divided into two major

subdivisions: autonomic and somatic. The autonomic nervous system (ANS) is largely

autonomous (independent) in that its activities are not under direct conscious control. It is concerned

primarily with visceral functions such as cardiac output, blood flow to various organs, and digestion,

which are necessary for life. The somatic division is largely concerned with consciously controlled

functions such as movement, respiration, and posture. Both systems have important afferent

(sensory) inputs that provide information regarding the internal and external environments and

modify motor output through reflex arcs of varying size and complexity.

The nervous system has several properties in common with the endocrine system, which is

the other major system for control of body function. These include high-level integration in the brain,

the ability to influence processes in distant regions of the body, and extensive use of negative

feedback. Both systems use chemicals for the transmission of information. In the nervous system,

chemical transmission occurs between nerve cells and their effector cells. Chemical transmission

takes place through the release of small amounts of transmitter substances from the nerve terminals

into the synaptic cleft. The transmitter crosses the cleft by diffusion and activates or inhibits the

postsynaptic cell by binding to a specialized receptor molecule.

By using drugs that mimic or block the actions of chemical transmitters, we can selectively

modify many autonomic functions. These functions involve a variety of effector tissues, including

cardiac muscle, smooth muscle, vascular endothelium, exocrine glands, and presynaptic nerve

terminals. Autonomic drugs are useful in many clinical conditions. However, a very large number

of drugs used for other purposes have unwanted effects on autonomic function.

TABLE-ADRENERGIC AGONIST

EPINEFRIN

(A)

NE

(B)

PHENYL

EFRIN

(C)

DOPAMINE

(D)

TERBUTALIN/

ALBUTEROL

(E)

Affinity/

Selectivity

α1,2-β1,2

β dominant

,1>> 2

dominant

1>2>>>> D1=D2>> >> 2>1 >>>>

BP:

Systolic

Diastolic

↑ (β1)

↓ slightly

↑ (β1)

↑

-

↑(?)

↑ (β1)

?

-

↓

Heart Ino (+) Chrono (+)

Ino (+)

Chrono (+)

- Ino (+)

Chrono (+)

Palpitation +/-

Bronchus Dilatation Dilatation - - Dilatation

Urinary tract Sphincter int constriction

Sphincter int

constriction

Sphincter int

constriction

- -

Mtbl :CH/lipid Blood gluc ↑ - - - Blood gluc ↑

Pupil Mydriasis IOP ↓ (β)

- mydriasis - -

Adverse reaction CNS disturbances: anxiety, fear, tension,

= epinefrin Hypertension Sympathetic

stimulation

Palpitation

headache, tremor

Cerebral hemorrhages

Arrhytmias

Pulmonary edema

Indication Bronchospasm

Anaphylactic shock

Glaucoma Local

anesthetic

:DOA

Shock

Decongestant

Tachycardia (?)

Cardiac

stimulant

Bronchospasm

Uterine

contraction

Contraindication Hypertension Tachycardia Etc.

Hypertension

Hypertension

- Hypotension

Note: - : not directly affected

TABLE-ADRENERGIC ANTAGONIST FENTOL-

AMIN

(F)

PRAZOSIN/

TERAZOZIN

(G)

PROPRA-

NOLOL

(H)

ATE-

NOLOL

(I)

PIN-

DOLOL

(J)

LABETALOL/

CARVEDILOL

(K)

Affinity/

Selectivity

1= 2

1>>>> 2

1

(Cardio-

selectif)

ISA (+)

+ 1

BP:

Systolic

Diastolic

-

-

↓

↓

↓

↓

↓

-

↓

↓ slightly

↓

↓

Heart - - ↓ ↓ ↓ slightly ↓

Bronchus - - constriction - Slightly

constriction

-

Uterus - - - - - -

Urinary

tract

Sphincter int

dilatation

Sphincter int

dilatation (?)

- - - Sphincter int

dilatation

Mtbl :

CH/lipid

- - Hypo glycemia hypoglycemia

Pupil constriction constriction - - - ?

Adverse

reaction

(AR)

Tachycardia Post

ural

Nasal –congestion

Fluid- retention

Bronchoconstric

tion

Increased Na+

retention

Hypoglycemia

< < Orthostatic

hypotension

Dizziness

Hypotension GI –

stimulation

GI – Hypermotility

Postural Hypotension

Hypotension

Bradycardia

Fatigue

Drowsiness

Sexual

impairment

Indication Frostbite Hypertension Hypertension

Glaucoma:

IOP

Migraine

Hyper

thyroidsm

Angina pectoris

Myocardial

infarction

Hypertensio

n Hypertension Hypertension

Contraindic

ation

= AR =AR =AR ? ? AR

Note: - : not directly affected

TABLE – CHOLINERGIC AGONIST

Affinity/

Selectivity

Bethanechol

(L)

Physostigmine

(M)

Ach esterase

inhibitor

Neostigmine

(N)

Ach esterase

inhibitor

Endrophonium

(O)

Ach esterase inhibitor

Muscarinic

Nicotinic

+

+

+ :ANS & NMJ

NM

junction

- Tonus ↑

Depolarization

↑

Tonus ↑

Depolarization

↑

Tonus ↑

Depolarization ↑

BP Neg

(th/dose)

Neg (th/dose) (th/dose)↓ (th/dose) ↓

Heart

≠ : Chrono +

ino (-)

Chrono (-)

Inotropic (-)

Chrono (-)

Inotropic (-)

Chrono (-)

Inotropic (-)

Bronchus Constriction Constriction Constriction Constriction

Urinary

tract

Ureter cont Ureter cont Ureter cont Ureter cont (?)

GIT

- Motility

- Secretion

↑

Stimulation

↑

Stimulation

↑

Stimulation

↑

Stimulation

MTBL - - - -

Pupil Miosis miosis miosis miosis

Adverse

reaction

Nausea-

vomit

Diarrhea

Abdominal

pain

Sweating

Salivation

Broncho-

constriction

↓ BP

Contraction

skeletal muscle

M)

Cholinergic

intoxication

Muscle

weakness,

cramps,

fasciculation

(N)

HR ↓

Contraction

skeletal

muscle (M)

Cholinergic

intoxication

Muscle

weakness,

cramps,

fasciculation

(N)

BP ↓

Contraction skeletal muscle (M)

Cholinergic intoxication

Muscle weakness, cramps,

fasciculation (N)

Indication Atonic

bladder

Glaucoma

UT-GI atony

Overdoses of

atropine, TCA,

phenotiazin

(enter CNS)

Myasthenia

gravis

Glaucoma

GI & UT atony

Antidote for

neuromusc

blocker

Myasthenia gravis

Contra

indication

Peptic ulcer

Asthma

Cardiac dis.

Parkinsonian

Hyperthyroid

(predispose

to arrhytmia)

Obstruction

of GI & UT

Convulsion

(high dose)

Peptic ulcer

Asthma

Cardiac dis.

Parkinsonian

Hyperthyroid

(predispose to

arrhytmia)

Obrstuction of

GI & UT

Peptic ulcer

Asthma

Cardiac dis.

Parkinsonian

Hyperthyroid

(predispose to

arrhytmia)

Obstruction of

GI & UT

Peptic ulcer

Asthma

Cardiac dis.

Parkinsonian

Hyperthyroid (predispose to

arrhytmia)

Obstruction of GI & UT

Note: - : not directly affected

TABLE – CHOLINERGIC ANTAGONIST & NEUROMUSCULAR BLOCKERS Atropine/scopolamine

(P)

Tubocurarine / Succinylcholine

(Q)

Affinity/ Selectivity Antimuscarinic

(central-peripheral)

NM blockers

NM junction - + : skeletal musc. :↓ constraction

paralysis

BP - -

Heart Dose <: ↓ HR (vagal activation)

Dose >: ↑ HR (M)

- tachycardia?? - Contractility↓

Salivary gland ↓ -

Urinary tract Reduced motility -

GIT - Motility - Secretion

Reduced - (exc. Pirenzepine: M1 antagonist)

-

MTBL - -

Pupil Mydriasis Unpredictable: loss of vision, moderate

dilation

Adverse reaction Dry mouth Blurred vision /mydriasis Tachycardia Constipation, urinary retention CNS: confuse, delirium, hallucination Glaucoma

Malignant hyperthermia (succinylcholine)

Muscular rigidity

Indication Cyclopegic Antispasmodic (GI/UT) Overdose of organophosphate Mushrooms poisoning Antisecretory prior to surgery Scopolamine: motion sickness Parkinson dis.

Muscle relaxant in general anesthesia

Facilitate intubation

Contra indication Glaucoma

Others related to AR

Related to its AR

Note: Ganglionic blockers: Trimethaphan, Mecamylamine ↓ BP instantly - : not directly affected

Activity 2: Poster

POSTER 1

1 2

3

4

6

5

POSTER 2

POSTER 3

POSTER 4

1

2

3

1

2

3

4

5

6

7

8

9

10

11

12

13

14

POSTER 5

POSTER 6

Activity 3: Case Discussion

CASES

G Refferences

Roger J. porter & Brian S. meldrum in Katzung BG. Basic and Clinical Pharmacology.

11th Edition. Lange Medical Books/McGraw-Hill. 2009. Chapter 6

ADRENOCEPTOR

ALPHA 1 ALPHA 2 BETA 1 BETA 2